Obesity and hyperlipidemia are often associated with insulin resistance, diabetes mellitus, hypertension, and cardiovascular diseases, resulting in a high morbidity rate and early mortality. Little is known about the etiology of obesity and hyperlipidemia. The current strategy involves weight control. Several alternate new therapeutic approaches include the use of β3-adrenoceptor agonists, CCK-A/cholecystokinin-A-receptor agonists, neuropeptide Y-receptor antagonists and pancreatic lipase inhibitors. The pancreatic lipase inhibitors (orlistat/lipstatin) are among the best candidates.
Lipstatin is a precursor for Orlistat. Upon hydrogenation, lipstatin is converted to form Orlistat. Orlistat has the chemical name (2S, 3S, 5S)-5-[(S)-2-formamido-4-methylvaleryloxy]-2-hexy-3-hydroxyhexadecanoic acid lactone [a/k/a “N-formyl-L-leucine ester with (3S, 4S)-3-hexyl-4-[(2S)-2-hydroxytridecyl]-2-oxetanone”, (−)-tetrahydrolipstatin, tetrahydrolipstatin, and orlipastat]. Orlistat has the following chemical formula: 